CAS: 521284-22-0; (1R)-2-{[2-(4-Aminophenyl)Ethyl]Amino}-1-Phenylethanol Hydrochlor Ide (1:1)

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CAS号521284-21-9 (alphaR)-alpha-... | CAS号223673-61-8 米拉贝隆

D-扁桃酸置于sodium Tetrahydroborate,硼酸三甲酯,氢气,N,N-二异丙基乙胺体系中,用 四氢呋喃,甲醇,乙腈 作为反应溶剂,化学反应 21.0H,反应生成 米拉贝隆中间体
参考文献:期间加入nabh的规模扩大的不明杂质的系统的调查显着的形成金额4-I 2的mirabegron硝基酰胺中间体的介导还原#
标题:期间加入nabh的规模扩大的不明杂质的系统的调查显着的形成金额4-I 2的mirabegron硝基酰胺中间体的介导还原#
摘要:在实验室规模成功开发了mirabegron(1)的制造工艺之后,在批量生产过程中出现了混乱的局面,其中硼氢化钠-碘(nabh 4-I 2)介导的硝基酰胺4还原结束在硝基胺中间体5中添加大量(〜10%)未指明的杂质.通过对结构的阐明和细致的研究,确定了其在反应生成过程中的反应路径,并提出了阻止其形成的有效机制.nii 2(腐蚀产物)与nabh 4的反应原位反应生成的硼化镍(ni 2 B)随后发现thf(溶剂)的亲电腐蚀是形成杂质(8A)的原因.通过适当控制执行后续批次,可以制止这种杂质,并成功地为mirabegron提供了所需的质量.
DOI:10.1021/acs.Oprd.9B00365

专利信息

专利号:US-9815771-B2
优先权日:2014-08-06
标题 :Method for the synthesis of mirabegron and its derivatives
发明人：MARQUILLAS OLONDRIZ FRANCISCO; RIEGO ARBOLEYA ESTELA
权利人:INTERQUIM SA
摘要:The present invention refers to a method for the synthesis of a compound of formula (I), solvates, stereoisomers or salts thereof, a key intermediate in the synthesis of Mirabegron by reduction of an amide in the presence of an amine-boranecomplex, wherein the amine is an aniline.

专利号:US-7982049-B2
优先权日:2001-10-30
标 题:α-form or β-form crystal of acetanilide derivative
发明人：KAWAZOE SOUICHIROU; SAKAMOTO KENICHIROU; AWAMURA YUJI; MARUYAMA TATSUYA; SUZUKI TAKAYUKI; ONDA KENICHI; TAKASU TOSHIYUKI
权利人:ASTELLAS PHARMA INC
摘要:To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with α-form crystal and β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide. The α-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The β-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the α-form crystal.

专利号:ES-2676586-T3
优先权日:2014-08-06
标题 :Procedure for the synthesis of mirabegron and its derivatives